采用亲和色谱法研究了β2-肾上腺素受体(β2-AR)与中药活性小分子盐酸巴马汀(Pa)和盐酸药根碱(Ja)的相互作用.前沿色谱法说明Pa与β2-AR之间存在一类结合位点,Ja与β2-AR之间存在两类结合位点.在pH 7.4,25℃时,用竞争洗脱法测得了Pa与β2-AR的结合常数为2.93×104 L?mol-1,结合位点浓度为1.13×10-4 mol?L-1,Ja在β2-AR低、高亲和力位点上的结合常数分别为1.93×104和1.56×105 L?mol-1,对应的结合位点浓度分别为1.25×10-4 mol?L-1和1.00×10-5 mol?L-1,两类结合位点数的比值为93∶7,且Pa和Ja在低亲和力位点上存在竞争作用.热力学研究表明,静电力是这两种药物与β2-AR之间作用的主要驱动力.
The interaction of two bioactive components of Chinese traditional herb,palmatine(Pa) and jatrorrhizine(Ja),with β2-adrenoceptor(β2-AR) was investigated by high-performance affinity chromatog-raphy.The binding isotherms of two drugs were determined by frontal analysis,and the results showed that Pa had one kind of binding site,and Ja had two kinds of binding sites on β2-AR molecular.The association constants and binding sites were determined by zonal elution,at pH 7.4 and 25 ℃.The association constant for Pa was 2.93×104 L?mol-1,and the concentration of the binding sites was 1.13×10-4 mol?L-1.The as-sociation constants for Ja at the low and high binding sites were 1.93×104 and 1.56×105 L?mol-1,and the concentration of the two binding sites were 1.25×10-4 and 1.00×10-5 mol?L-1,respectively.The ratio of two binding sites was 93∶7.It was further proved that Pa and Ja competed the low binding site on β2-AR.Thermodynamic results indicated that the interaction between the two drugs and β2-AR was mainly drived by electrostatic force.